Figure 1.

TRAIL formulations with increased bioactivity for cancer treatment. Different formulations of TRAIL using distinct experimental approaches have been developed to increase its therapeutic potential. These formulations are mainly based in fusion proteins with single-chain variable antibody fragments (scFv), conjugation with nanoparticles and, cell-based methods to express and/or secrete Apo2L/TRAIL. The main properties improved with these highly bioactive formulations are the increase of the molecule stability, tumor targeting and the possibility of combination with other antitumor agents in a unique formulation. References: 1: leucine zipper-TRAIL;^{8, 142} 2: Isoleucine zipper-TRAIL homotrimer;³⁰ 3: PEG-HZ-TRAIL;^{150, 152} 4: APG350;²⁰⁹ 5: Fn14:TRAIL;^{192, 193} 6: TRAIL HSA-NPs;¹⁵³ 7: PEG-TRAIL microspheres;^{152, 169} 8: TRAIL-PEG-NPs;¹⁵⁴ 9: TRAIL-LPs;^{173, 174, 176} 10: PEG-TRAIL/Dox microspheres;¹⁵¹ 11: TRAIL/Dox HSA-NPs;¹⁶⁷ 12: magnetic NPs-TRAIL;¹⁷⁰ 13: LUV-TRAIL;^{67, 171, 172, 212} 14: LUV-Apo2L.0;²¹³ 15: sTRAIL-targeted stealth liposome;¹⁷⁹ 16: TRAIL/Tf/Dox HSA-NPs;¹⁶⁸ 17: immuno-LipoTRAIL;¹⁷⁷ 18: Anti-CD3:TRAIL K12:TRAIL;¹⁹⁶ 19: leukocytes coated with LUV-TRAIL-ES;¹⁷⁸ 20: granulocytes coated with CLL1:TRAIL;²⁰² 21: MBOS4:TRAIL;⁶⁹ 22: scFv425:sTRAIL;^{189, 190} 23: scFvCD19:sTRAIL;¹⁸⁵ 24: Db_αEGFR-scTRAIL;¹⁴⁵ 25: scFvCD33:sTRAIL;¹⁸⁶ 26: Anti-MCSP:TRAIL;¹⁸⁸ 27: scFv-EHD2-scTRAIL;²¹¹ 28: scFvG28:TRAILmutRs;¹⁹⁵ 29: scFvCD70:TRAILmutRs;⁷⁰ 30: RGD-L-TRAIL;²⁰³ 31: CD40ed:TRAILed;²¹⁴ 32: MSC.scFvCD20-sTRAIL;¹⁸⁷ 33: ANG-CLP/PTX/pEGFP-hTRAIL;¹⁷⁶ 34: sTRAIL-expressing E. coli DH5α²¹⁵